Low Dose Naltrexone (LDN) has emerged has an effective treatment for many chronic health conditions, pain management and autoimmune conditions. Naltrexone is a medication that was originally used to help manage alcohol and opioid addiction by preventing the “high” caused by these substances. It is now also used in low doses, termed Low Dose Naltrexone to treat a variety of conditions, with good health outcomes for patients.

What is naltrexone?

Naltrexone is a compounded medication first discovered in the 1980s by a physician in New York City, Dr Bahari. It was originally developed and FDA approved for use in alcohol and drug addiction.

It helps narcotic dependents who have stopped taking narcotics to stay drug-free and alcoholics stay alcohol-free. It is used as part of an overall program that may include counselling, attending support group meetings, and other treatment recommended by a patient’s treating doctor.

Naltrexone is not a narcotic. Instead, blocks the effects of narcotics and alcohol, stopping you from feeling high. It doesn’t produce any narcotic-like effects or cause mental or physical dependence and doesn’t prevent patients from becoming impaired while drinking alcohol. (1)

When realising how therapeutic naltrexone was for patients, Dr Bahari, turned his attention to other patients and started using the medication in smaller doses with his HIV/AIDS and cancer patients.(2) He noticed that for these patients, a much lower dose of naltrexone (about 3 milligrams) had beneficial immune-modulating effects. This discovery gave rise to a grassroots movement of patients and practitioners who had seen LDN work and were calling for additional research and mainstream attention.(3)

Now, naltrexone is used in low dosage form to treat patients with a wide variety of conditions and diseases, including chronic diseases and autoimmune disorders.

What is low-dose naltrexone?

Low-dose naltrexone, also known as LDN, is taken in doses much smaller than the size of a traditional dose, usually less than 5 milligrams per day.

When it is used as a medication for something other than what it was approved to treat, it is known as an off-label use. Although clinical research has shown that the use of LDN is effective for many patients, being an off-label use medication means it hasn’t gone through the same amount of rigorous testing to confirm its effectiveness and safety for treating these other conditions.

How does it work?

LDN works as an opioid antagonist, and among other mechanisms, works to boost the body’s endorphins and enkephalins. In low doses, it releases endorphins over an extended period of time.

This rise in feel-good hormones contributes to the reduction of inflammation and an improvement of immune function, and often minimizes the symptoms and progression of chronic disease.

It also works to promote healing, inhibit abnormal cell growth, and provide relief of pain. The side effects are minimal and often transient.

The LDN Trust summarises LDN’s mechanism of action as:

“Levo-Naltrexone is an antagonist for the opiate/endorphin receptors

This causes increased endorphin release
Increased endorphins modulate the immune response
This reduces the speed of unwanted cells growing. Dextro-Naltrexone is an antagonist for at least one, if not more, immune cells
Antagonises “TLR,” suppressing cytokine modulated immune system
Antagonises TLR-mediated production of NF-kB – reducing inflammation, potentially downregulating oncogenes” (4)

This means that, independent of the opiate-antagonist pathway, LDN also works to suppress microglial activity. “Microglia are the primary immune cells in the central nervous system and are responsible for creating inflammation in response to pathogens or injury. When activated, microglia secrete factors such as pro-inflammatory cytokines, prostaglandins, nitric oxide, and excitatory amino acids.” (5)

Dextro-naltrexone is a different form of naltrexone which may be more effective at reducing neuroinflammation and produces fewer side effects. Dextro-Naltrexone is an antagonist for at least one, if not more immune cells.

How does LDN make you feel?

As LDN may increase endorphins (morphine like substances produced by the body), it can result in a feeling of well-being. Human trials have demonstrated improvement in mood and in quality-of-life scores. This feeling helps lower stress, reduce depression, and increase healing.

LDN has historically been prescribed at bedtime as the majority of endorphin production in our body occurs in the middle of the night. However, some individuals may experience sleep disturbances with night-time dosing and in these cases, taking LDN in the morning may be suggested by the prescribing doctor. When you are prescribed LDN, you treating physician or Functional Medicine health practitioner will ensure the timing and dosage is correct for you.

Types of LDN

Liquid – the most commonly used type of LDN. It is taken daily and dosed using a baby oral syringe.
Capsules or tablets – available in a variety of strengths
Sublingual drops – designed for patients with problems taking medications orally, or for people who want to guarantee the fastest delivery of the drug into their bloodstream. A number of drops are placed under the tongue from a dropper bottle and dose is increased and decreased by the number of drops taken.
Creams and topical lotions
Eye drops
Tablets

What conditions can it treat?

LDN is now used to treat a wide variety of conditions, including:

Autoimmune Conditions
Cardiac diseases
Chronic pain
Skin diseases
Ear, nose and throat conditions
Endocrine diseases
Gastrointestinal diseases
Haematologic diseases
Hepatology
Immunology
Infectious diseases
Cancer
Neurologic diseases
Eye diseases
Paediatric disorders
Psychological disorders
Lung disease
Kidney and urologic diseases
Arthritis and autoimmune disorders
Sleep disorders
Vasculitis
Women’s health (6)

LDN and the treatment of chronic disease

There has been a growing body of evidence that the body’s endorphins have a critical role in regulating the immune system and providing pain relief. One of the most exciting aspects of LDN is the low reported incidence of adverse side effects, although the one side effect often reported is vivid dreaming and sleep disturbances. (7)

Low-dose naltrexone (LDN) has been demonstrated to reduce symptom severity in conditions such as fibromyalgia, Crohn’s disease, rheumatoid arthritis, multiple sclerosis, lupus, cancer, depression/anxiety, irritable bowel syndrome, Hashimoto’s hypothyroidism and complex regional pain syndrome.

As LDN has an effect of increasing regulation of the immune system, it can be especially helpful for people suffering from the effects of a dysregulated immune system. “Chronic pain syndromes, autoimmune disease, and fibromyalgia are a few conditions attributed to unregulated inflammation and attacks on “self” tissues.” (7)

The most researched conditions treated by LDN include:

One of the most heavily researched applications of LDN is in the treatment of fibromyalgia. In one trial, LDN reduced fibromyalgia symptoms by 30% over a placebo, improved patients’ tolerance to heat and touch and had very few adverse side effects.(9) In another clinical trial, LDN improved patients’ pain, mood and quality of life significantly better than a placebo. For fibromyalgia patients living with chronic pain, this treatment is safe and often effective. (10)
The effectiveness of reducing multiple sclerosis (MS) symptoms is still being determined although in one study (11), LDN substantially improved quality of life in multiple sclerosis patients, and in another trial,(12) it reduced participants’ fatigue and depression with only mild side effects like sleep disturbances, agitation and urinary tract infections.
Some research(13) has also focused on LDN as a potential treatment for Crohn’s disease. focused on children aged 8-17, it seemed to reduce disease activity and even prompt remission. After 16 weeks, 25% had achieved remission and 67% showed improvement. (14)

Side effects

“Full-dose naltrexone” may cause the following side effects:

nausea and vomiting
abdominal pain
constipation
decreased appetite
headache
fatigue
insomnia
dizziness
depression
anxiety

These risks fall significantly when taking a lower dose, with minor, or no, side effects reported.

You shouldn’t take LDN if you:

take opioid medications
are in an opioid maintenance program
are in acute opiate withdrawal
have liver problems

Remember, LDN for the treatment of chronic disease is considered an off-label use. It’s very important to talk to your doctor before trying it to ensure it won’t interact with any other medications you may be taking.

You should also never try to create your own dosage of naltrexone tablets to create LDN on your own. At Advanced Functional Medicine, we will ascertain if LDN is the right treatment for you, what the approach should be and the correct dosage to help you combat symptoms of your condition.

Additionally, avoiding inflammatory foods such as processed sugar, wheat, gluten, alcohol and dairy with a balanced lifestyle, possibly a paleo-type diet and exercise, will bring optimal results.

How we can help

Clinical research to date suggests that LDN is a promising treatment approach for chronic diseases. As LDN is relatively inexpensive and has few side effects, it is very possible that it will eventually come to be seen as one of the most promising treatments for many chronic diseases.

At Advanced Functional Medicine, we work with patients to ascertain the right dosing strategy to treat your particular condition. Some patients find success quickly, while others may need to try a variety of dosing strategies, which may take up to several months to achieve success. A number of our patients have found relief from their long standing chronic conditions and pain through Low Dose Naltrexone while some haven’t benefitted noticeably and haven’t continued.

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How low dose naltrexone could benefit your health condition